Theobromine for the Treatment of Cough

a technology of theobromine and cough, applied in the field of theobromine, can solve the problems of doubtful effectiveness and distressing persistent cough, and achieve the effects of reducing side effects and drug burden, reducing sedation, and reducing the burden of drugs

Inactive Publication Date: 2012-05-24
INFERST KHEHLTKEHR LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006]The invention is based at least in part on data showing an equivalent anti-tussive effect for inhaled theobromine at ⅓ of the oral dose in a citric acid-induced cough model. Via the inhaled route, theobromine is surprisingly potent and does not follow the oral PK / PD relationship, revealing that theobromine has a substantially local effect in the lung. Consequently, via the inhaled route, less drug is given for an equivalent oral effect, so reducing side-effects and drug burden. Side-effects such as sedation can be minimised.
[0007]Theobromine can be used in combination or co-administration with a wide range of respiratory medicines, with little concern over systemic complications that may arise. Theobromine can be administered on a continued basis without concern over systemic side-effects (e.g. tachycardia). Theobromine can be administered on a once daily basis.

Problems solved by technology

Persistent cough can be distressing.
Over-the-counter remedies are available but their effectiveness is doubtful.

Method used

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  • Theobromine for the Treatment of Cough
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Examples

Experimental program
Comparison scheme
Effect test

example

[0029]The aim of this Example is to provide an assessment of the antitussive activity of intra-tracheally (i.t.) or orally dosed (p.o.) administered theobromine (3-30 mg / kg) compared to the positive control codeine (25 mg / kg, i.p.) against irritant-induced cough responses.

Animals

[0030]Male Dunkin Hartley guinea pigs (350-550 g, supplied by Harlan UK Ltd) were used throughout the study.

Protocol

[0031]Thirty-six guinea pigs were randomly allocated to one of the six treatment groups (see Table 1) according to the blinding code. The blinding code was not revealed to the experimenter until coughs from all of the animals had been tallied.

[0032]Guinea pigs were dosed intra-tracheally with theobromine or vehicle, orally with theobromine and intra-peronteneally with codeine. All pre-treatments were administered at t−30 min prior to citric acid exposure.

[0033]Individual guinea pigs were placed in an exposure chamber with an airflow of 2 L / min at t−10 min prior to citric acid exposure to acclim...

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Abstract

The present invention is theobromine as an active agent to be delivered via the inhaled route, for the treatment of cough.

Description

FIELD OF THE INVENTION[0001]This invention relates to theobromine and its use in the treatment of cough.BACKGROUND OF THE INVENTION[0002]Cough is a protective reflex. Persistent cough can be distressing. Over-the-counter remedies are available but their effectiveness is doubtful.[0003]WO98 / 42322 discloses the use of theobromine for the treatment of cough, to be given orally. It shows the anti-tussive activity of oral theobromine which is directly correlated to its plasma concentration.[0004]Usmani et al., FASEB J. express article 10.1096, discloses that theobromine inhibits sensory nerve action and cough. Data are provided, showing effects following oral dosing in citric-acid induced cough in the guinea pig, in the capsaicin cough challenge in humans, and following bathing of isolated guinea pig vagus nerve preparations.SUMMARY OF THE INVENTION[0005]The present invention relates to the use of theobromine by inhalation, in the treatment of cough.[0006]The invention is based at least ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/522C07D473/10A61P11/14A61K9/14
CPCA61K31/522A61K9/0075A61P11/14
Inventor BREW, JOHNBANNISTER, ROBIN MARK
Owner INFERST KHEHLTKEHR LTD
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